- Synthetic method 4 - alkoxyphenol compounds
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The invention discloses a synthetic method of 4 - alkoxyphenol compounds, and belongs to the field of organic chemical synthesis. The method is as follows: An aryl alkyl ether compound is added to the sealing tube. The catalyst dimerization acetic acid rhodium and the oxidizing agent iodobenzene diethyl ester are added, a solvent trifluoroacetic anhydride is added, and the 4 -alkoxyphenol compound is prepared by heating reaction. To the invention, high regioselectivity direct hydroxylation of the aryl alkyl ether compound is realized, the application range of the substrate is wide, the yield is high, the activity after amplification reaction does not significantly decay, and higher yield is still obtained. The utility model has good practicability and industrial application prospect.
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Paragraph 0064-0066
(2021/09/29)
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- Para -Selective hydroxylation of alkyl aryl ethers
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para-Selective hydroxylation of alkyl aryl ethers is established, which proceeds with a ruthenium(ii) catalyst, hypervalent iodine(iii) and trifluoroacetic anhydride via a radical mechanism. This protocol tolerates a wide scope of substrates and provides a facile and efficient method for preparing clinical drugs monobenzone and pramocaine on a gram scale.
- Zhu, Runqing,Sun, Qianqian,Li, Jing,Li, Luohao,Gao, Qinghe,Wang, Yakun,Fang, Lizhen
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supporting information
p. 13190 - 13193
(2021/12/16)
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- Method for synthesizing herbicide clodinafop-propargyl key intermediate
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The invention discloses a method for synthesizing a herbicide clodinafop-propargyl key intermediate. According to the method, methyl 2-chloropropionate and hydroquinone are used as starting raw materials, under the catalytic action of inorganic alkali, nucleophilic substitution reaction is conducted, and methyl (R,S)-2-(4-hydroxyphenoxy)propionate is obtained; the generated methyl (R,S)-2-(4-hydroxyphenoxy)propionate is subjected to resolution hydrolysis reaction under the action of aspergillus oryzae WZ007, and a methyl (R)-(+)-2-(4-hydroxyphenoxy)propionate product is obtained; the generatedproduct is subjected to hydrolysis reaction continuously to obtain a target product R(+)-2-(4-hydroxyphenoxy)propionic acid. The synthesis method is simple; in the synthesis process, thalli of the aspergillus oryzae WZ007 are used for catalyzing selective hydrolysis of a methyl (R,S)-2-(4-hydroxyphenoxy)propionate substrate, thus the R-configuration ester and the S-configuration acid are obtained, the purpose of resolution is achieved, moreover, the raw materials of the method are cheap, the production cost is low, and the economic performance is good, so that the method has good applicationprospects.
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Paragraph 0049
(2018/11/27)
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- 6-chlorobenzoxazoloxy phenoxyacrylamide compounds and application thereof
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The invention discloses 6-chlorobenzoxazoloxy phenoxyacrylamide compounds and an application thereof as herbicides; the compounds are represented by the general formula (I), wherein W is selected fromC1-4 alkylene. The compounds not only have excellent he
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Paragraph 0058-0061
(2018/06/04)
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- 6-chlorobenzoxazol-oxyphenoxy propionate compound and application thereof
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The invention belongs to the field of herbicides and particularly relates to a 6-chlorobenzoxazol-oxyphenoxy propionate compound and application thereof. The compound is shown in a general formula (I). The compound provided by the invention not only has e
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Paragraph 0066-0069
(2017/08/18)
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- Synthesizing method for (R)-(+)-2-(4-hydroxy phenoxy) methyl propionate
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The invention discloses a synthesizing method for (R)-(+)-2-(4-hydroxy phenoxy)methyl propionate.The synthesizing method comprises the following steps that firstly, hydroquinone and a sodium hydroxide aqueous solution are put into a reaction kettle for a reaction, and a mixed solution containing p-hydroxyl sodium phenolate is generated; secondly, methyl 2-chloropropionate is added into the reaction kettle for a substitution reaction, and a mixed solution containing (R)-(+)-2-(4-hydroxy phenoxy)methyl propionate is generated; thirdly, an extraction solvent is added in the reaction kettle for extraction laying treatment, and then oil layer distillation treatment is carried out; fourthly, the mixed solution, obtained after oil layer distillation treatment, containing (R)-(+)-2-(4-hydroxy phenoxy)methyl propionate is cooled, crystallized, centrifuged and dried.The synthesizing procedures of the synthesizing method are simple, the product quality is good, the yield is high, and obtained MAQ is a white crystalline solid.
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Paragraph 0005; 0016
(2017/04/03)
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- Synthesis and biological evaluation of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists
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Free fatty acid receptor 1 (FFA1) is a new potential drug target for the treatment of type 2 diabetes because of its role in amplifying glucose-stimulated insulin secretion in pancreatic β-cell. In the present studies, we identified phenoxyacetic acid derivative (18b) as a potent FFA1 agonist (EC50 = 62.3 nM) based on the structure of phenylpropanoic acid derivative 4p. Moreover, compound 18b could significantly improve oral glucose tolerance in ICR mice and dose-dependently reduced glucose levels in type 2 diabetic C57BL/6 mice without observation of hypoglycemic side effect. Additionally, compound 18b exhibited acceptable PK profiles. In summary, compound 18b with ideal PK profiles exhibited good activity in vitro and in vivo, and might be a promising drug candidate for the treatment of diabetes mellitus.
- Wang, Xuekun,Zhao, Tianxiao,Yang, Baowei,Li, Zheng,Cui, Jian,Dai, Yuxuan,Qiu, Qianqian,Qiang, Hao,Huang, Wenlong,Qian, Hai
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p. 132 - 140
(2015/02/18)
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- Resolution of (R, S)-ethyl-2-(4-hydroxyphenoxy) propanoate using lyophilized mycelium of Aspergillus oryzae WZ007
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The mycelium of Aspergillus oryzae WZ007 was successfully developed to kinetic resolution of (R, S)-ethyl-2-(4-hydroxyphenoxy) propanoate ((R, S)-EHPP) for production of (R)-ethyl-2-(4-hydroxyphenoxy) propanoate ((R)-EHPP). The key biocatalytic process parameters (pH, temperature, rotation speed and substrate concentration) were optimized. Under the optimum conditions, the optical purity of (R)-EHPP was improved up to >99% when the conversion was above 49%. A. oryzae WZ007 whole-cell lipase exhibited high reaction capacity, enantioselectivity and good reusability. The tolerable substrate concentration was 0.5 mol/L, and dry mycelium of A. oryzae WZ007 maintains over 80% of its initial activity after eight repeating cycles. Therefore the enzymatic preparation of (R)-EHPP route was suitable for industrial application.
- Zheng, Jian-Yong,Wu, Jia-Yu,Zhang, Yin-Jun,Wang, Zhao
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- COMPOUNDS AND COMPOSITIONS AS PPAR MODULATORS
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The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families.
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Page/Page column 54
(2010/11/27)
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- Design and synthesis of potent and subtype-selective PPARα agonists
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Beginning with a moderately potent PPARγ agonist 9, a series of potent and highly subtype-selective PPARα agonists was identified through a systematic SAR study. Based on the results of the efficacy studies in the hamster and dog models of dyslipidemia and the desired pharmacokinetic data, the optimized compound 39 was selected for further profiling.
- Desai, Ranjit C.,Metzger, Edward,Santini, Conrad,Meinke, Peter T.,Heck, James V.,Berger, Joel P.,MacNaul, Karen L.,Cai, Tian-Quan,Wright, Samuel D.,Agrawal, Arun,Moller, David E.,Sahoo, Soumya P.
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p. 1673 - 1678
(2007/10/03)
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- A novel synthesis and herbicidal activity of fluorine-containing pyrazolo[3,4-d]pyrimidin-4-one derivatives
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The 6-(4-alkoxycarbonylalkoxy)phenoxy-3-alkylthio-5-(fluoro-substituted)phenyl-1-phenylpyrazolo[3,4-d]pyrimidin-4-ones 6 have been successfully synthesized via a tandem aza-Wittig and annulation reactions of the corresponding iminophosphorances 4, aromatic isocyanate, and substituted phenols 2 in 59-69% isolated yields using actonitrile as solvent. These novel compounds 6 could be oxidized to sulfones 7 by hydrogen peroxide in satisfactory yields (57-93%). Their structures were clearly verified by spectroscopic data (IR, 1H NMR, 13C NMR, MS, Elemental analysis or X-ray diffraction crystallography). The results of preliminary bioassay indicated that these compounds possess herbicidal activity against the root of rape and barnyard grass.
- Liu, Hui,Wang, Hong-Qing,Ding, Ming-Wu,Liu, Zhao-Jie,Xiao, Wen-Jing
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p. 1584 - 1590
(2008/09/18)
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- COMPOUNDS AND COMPOSITIONS AS PPAR MODULATORS
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The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPAR.
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Page/Page column 79
(2010/02/14)
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- Synthesis of 2-(4-hydroxyphenoxy) alkanoic acid esters
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A method for synthesizing 2-(4-hydroxyphenoxy)alkanoic acid esters by reacting a hydroxyaromatic ketone derivative with a 2-substituted alkanoic acid ester under basic conditions and thereafter oxidizing the intermediate with subsequent hydrolysis.
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- Process for the preparation of optically active 2-(4-methoxyphenoxy) propionic acid
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A process for the preparation of optically active 2-(4-methoxyphenoxy)propionic acid of at least 75 percent enantiomeric excess of the desired optical isomer comprised of contacting 2-chloropropionic acid or a lower alkyl ester or an alkali metal salt thereof, having an optical purity greater than 85 percent of the opposite configuration, with from 3 to 10 molar equivalents of 4-methoxyphenol in an aqueous base.
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- Quinoxalinyloxy ethers as selective weed control agents
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This invention relates to herbicidal quinoxalinyloxy ethers, herbicidal compositions containing said ethers, and methods of using said compounds as herbicides.
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- Preparation of monoalkylated dihydroxybenzenes
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Preparation of monoethers of dihydroxybenzenes from an alkenylphenol and an alkylating agent and thereafter oxidizing in the presence of an acid catalyst.
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- Monoalkylation of dihydroxy aromatic compounds
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There is disclosed a process for the reduction of the diether impurities formed when a dihydroxy aromatic compound is reacted with an alkylating agent in an alcoholic solvent in the presence of two to three equivalents of base. The diether impurities are removed by removing a quantity of the alcoholic solvent and adding a solvent into which the diether impurities may be extracted.
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- 2-Ethoxyethyl 2-(4-hydroxyphenoxy)-propanoate
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Preparation of monoethers of dihydroxybenzenes from an isopropenylphenol and an alkylating agent and thereafter oxidizing in the presence of an acid catalyst.
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- Benzotriazine derivatives as selective weed control agents
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This invention relates to herbicidal benzotriazine derivatives, herbicidal compositions containing said derivatives, and methods of using said derivatives as herbicides.
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